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公开(公告)号:US5126341A
公开(公告)日:1992-06-30
申请号:US684214
申请日:1991-04-12
申请人: Fumio Suzuki , Takeshi Kuroda , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe
发明人: Fumio Suzuki , Takeshi Kuroda , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe
IPC分类号: A61K31/435 , A61K31/00 , A61K31/4353 , A61K31/4375 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P37/08 , C07D471/04
CPC分类号: C07D471/04
摘要: Disclosed are naphthyridine derivatives represented by formula (I) ##STR1## wherein: X represents hydrogen; lower alkyl; aralkyl; substituted or unsubstituted aryl; substituted or unsubstituted aromatic heterocyclic group; --NR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 independently represent hydrogen or lower alkyl; ##STR2## wherein W represents N or CH, Z represents a single bond, oxygen or NR.sup.3 (wherein R.sup.3 represents hydrogen, lower alkyl or benzyl) and n1 and n2 represent an integer of 1 to 3; or substituted or unsubstituted thiazolinyl; andY is a single bond or alkylene and pharmaceutically acceptable salts thereof. The compounds show potent anti-inflammatory activity and are expected to be useful in treating rheumarthritis.
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公开(公告)号:US5192768A
公开(公告)日:1993-03-09
申请号:US757988
申请日:1991-09-12
申请人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
发明人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: A pyrazoloquinoline derivative having the formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, or a lower alkoxycarbonyl group; the dotted line means that the pyrazole ring has two conjugated double bonds; and R.sup.4 is bonded to the nitrogen atom at the 1-position or 2-position, or pharmacologically acceptable salts thereof. These compounds exhibit excellent anti-inflammatory activity and hepatic insufficiency treating activity.
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公开(公告)号:US5527908A
公开(公告)日:1996-06-18
申请号:US94106
申请日:1993-08-05
申请人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Soichiro Sato , Hiroshi Tanaka
发明人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Soichiro Sato , Hiroshi Tanaka
IPC分类号: C07D513/14 , A61K31/505
CPC分类号: C07D513/14
摘要: Pyrazolothiazolopyrimidine derivatives represented by the Formula ##STR1## and pharmaceutically acceptable salts thereof are useful as anti-inflammatory, analgesic, immunomodulatory and anti-ulcer agents.
摘要翻译: PCT No.PCT / JP92 / 01595 Sec。 371日期:1993年8月5日 102(e)日期1993年8月5日PCT提交1992年12月7日PCT公布。 公开号WO93 / 12120 PCT 日期:1992年6月24日。由式< IMAGE>表示的吡唑并噻唑并嘧啶衍生物及其药学上可接受的盐可用作抗炎,镇痛,免疫调节和抗溃疡剂。
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公开(公告)号:US5371225A
公开(公告)日:1994-12-06
申请号:US170192
申请日:1993-12-22
申请人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Kenji Ohmori , Hiroshi Nakajima , Tadafumi Tamura , Soichiro Sato
发明人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Kenji Ohmori , Hiroshi Nakajima , Tadafumi Tamura , Soichiro Sato
IPC分类号: A61K31/00 , A61K31/47 , A61K31/55 , C07D221/18 , A61K31/44
CPC分类号: C07D221/18
摘要: The present invention relates to novel tetracyclic compounds represented by formula (I) ##STR1## (wherein each of X.sup.1 and X.sup.2 independently represents hydrogen or lower alkyl; n represents an integer of 1 to 4), or a pharmaceutically acceptable salt thereof, which are useful as immunosuppressive agents.
摘要翻译: PCT No.PCT / JP93 / 00527 Sec。 371日期:1993年12月22日 102(e)日期1993年12月22日PCT 1993年4月23日PCT公布。 公开号WO93 / 22286 日本公开专利文献1:日本专利公开1 9 9 3年11月11日本发明涉及式(I)表示的新型四环化合物(Ⅰ)(其中X1和X2各自独立地表示氢或低级烷基; n表示1〜4的整数) ,或其药学上可接受的盐,其可用作免疫抑制剂。
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公开(公告)号:US5010084A
公开(公告)日:1991-04-23
申请号:US553551
申请日:1990-07-18
IPC分类号: A61K31/00 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61P11/00 , A61P11/06 , A61P11/08 , A61P37/00 , A61P37/08 , C07D471/04
CPC分类号: C07D471/04
摘要: Novel imidazoquinolone derivative represented by formula (I); ##STR1## wherein R.sup.1 represents lower alkyl or --(CH.sub.2).sub.m CO--R.sup.3 where R.sup.3 represents hydrogen, lower alkyl, hydroxy or lower alkoxy; and m is an integer of 1 to 3; R.sup.2 represents lower alkyl; or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US4994468A
公开(公告)日:1991-02-19
申请号:US489025
申请日:1990-03-05
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: Novel imidazoquinolone derivative represented by the formula (I); ##STR1## wherein R.sup.1 represents hydrogen, alkyl, cycloalkyl, alkenyl aralkyl, aralkenyl or substituted or unsubstituted aryl; X represents nitrogen or ##STR2## where R.sup.2 is hydrogen, hydroxyl, alkyl, cycloalkyl, alkenyl, aralkyl, aralkenyl, substituted or unsubstituted aryl, thiol, halogen, substituted or unsubstituted aromatic heterocyclic group, or --(CH.sub.2).sub.m CO.sub.2 R.sup.6 where R.sup.6 is hydrogen or lower alkyl and m is an integer of 0 to 3; Y represents oxygen or sulfur; R.sup.3 represents alkyl, cycloalkyl, alkoxyalkly, alkenyl, aralkyl, aralkenyl, --(CH.sub.2).sub.n -- Het where Het is substituted or unsubstituted aromatic heterocyclic group and n is an integer of 1 to 3 or --(CH.sub.2).sub.n CO.sub.2 R.sup.6a where n has the same meaning as defined above and R.sup.6a has the same meaning as defined as to R.sup.6 ; each of R.sup.4 and R.sup.5 independently represents hydrogen, lower alkyl, trifluoromethyl, cycloalkyl, halogen, hydroxyl, lower alkoxyl, lower alkylthio, nitro, amino, lower alkylamino, lower alkanoylamino, aroylamino, lower alkanoyl or aroyl; and a pharmaceutically acceptable salt thereof. The Compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.
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公开(公告)号:US5364859A
公开(公告)日:1994-11-15
申请号:US999658
申请日:1992-12-29
申请人: Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
发明人: Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
IPC分类号: A61K31/435 , A61K31/4375 , A61P11/08 , A61P29/00 , A61P37/08 , C07D471/14 , C07D487/04 , A61K31/53
CPC分类号: C07D471/14
摘要: Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX-Y-Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5) H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryl and pharmaceutically acceptable sails thereof.The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.
摘要翻译: 公开了由式(I)表示的咪唑并吡啶衍生物其中:R1表示低级烷基或取代或未取代的芳基; 并且XYZ表示其中R2表示氢,低级烷基,烯基,芳烯基或-C(R5)H-(CH2)n-R4(其中R4表示取代或未取代的芳基,取代或未取代的吡啶基,取代或未取代的呋喃基 ,羟基取代的低级烷基,低级烷酰氧基,吗啉代,低级烷酰基,羧基,低级烷氧基羰基,环烷基,羟基,低级烷氧基,卤素或NR6R7,其中R6和R7独立地表示氢或低级烷基; R5代表氢,低级烷基或苯基 ; n表示0〜3的整数)。 并且R 3表示氢,巯基,羟基,低级烷基或芳基及其药学上可接受的风帆。 这些化合物显示有效的抗炎,抗过敏和支气管扩张活性。
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公开(公告)号:US5219864A
公开(公告)日:1993-06-15
申请号:US847665
申请日:1992-03-04
申请人: Fumio Suzuki , Yoshikazu Miwa , Hiroaki Hayashi , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima
发明人: Fumio Suzuki , Yoshikazu Miwa , Hiroaki Hayashi , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima
IPC分类号: A61K31/44 , A61K31/4365 , A61P3/00 , A61P19/10 , A61P37/02 , A61P37/06 , A61P43/00 , C07D495/04
CPC分类号: C07D495/04
摘要: Disclosed is a thienopyridine derivative represented by formula (I): ##STR1## wherein one of A and B represents --S-- and the other represents --CH.dbd.; R represents hydrogen or lower alkyl, and Z represents pyridyl; or a pharmaceutically acceptable salt thereof.The thienopyridine derivative is useful as an immunoregulator and for the prevention and treatment of osteoporosis.
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公开(公告)号:US5468756A
公开(公告)日:1995-11-21
申请号:US241631
申请日:1994-05-12
申请人: Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
发明人: Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
IPC分类号: A61K31/435 , A61K31/4375 , A61P11/08 , A61P29/00 , A61P37/08 , C07D471/14 , C07D471/00 , A61K31/44
CPC分类号: C07D471/14
摘要: Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX--Y--Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5)H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryland pharmaceutically acceptable salts thereof.The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.
摘要翻译: 公开了由式(I)表示的咪唑并吡啶衍生物其中:R1表示低级烷基或取代或未取代的芳基; 并且XYZ表示其中R2表示氢,低级烷基,烯基,芳烯基或-C(R5)H-(CH2)n-R4(其中R4表示取代或未取代的芳基,取代或未取代的吡啶基,取代或未取代的呋喃基 羟基取代的低级烷基,低级烷酰氧基,吗啉代,低级烷酰基,羧基,低级烷氧基羰基,环烷基,羟基,低级烷氧基,卤素或NR6R7,其中R6和R7独立地表示氢或低级烷基; R5表示氢,低级烷基或苯基; n表示0〜3的整数)。 并且R 3表示氢,巯基,羟基,低级烷基或芳基及其药学上可接受的盐。 这些化合物显示有效的抗炎,抗过敏和支气管扩张活性。
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公开(公告)号:US5281610A
公开(公告)日:1994-01-25
申请号:US993920
申请日:1992-12-18
申请人: Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
发明人: Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
IPC分类号: C07D471/14 , A61K31/435 , C07D471/22
CPC分类号: C07D471/14 , Y10S514/88
摘要: Disclosed is a pyrazolonaphthyridine compound represented by the formula: ##STR1## wherein R.sup.1 is represents hydrogen, lower alkyl, aralkyl, or substituted or unsubstituted aryl, R.sup.2 represents hydrogen, lower alkyl, thienyl, substituted or unsubsutituted aryl, hydroxy or amino, or a pharmaceutically acceptable salt thereof.The compound possesses antiinflammatory effect, immunosuppressive effect, broncho-dilatory effect and hair growth-stimulative effect.
摘要翻译: 公开了由下式表示的吡唑并萘啶化合物:其中R 1表示氢,低级烷基,芳烷基或取代或未取代的芳基,R 2表示氢,低级烷基,噻吩基,取代或未取代的芳基,羟基或氨基,或 其药学上可接受的盐。 该化合物具有抗炎作用,免疫抑制作用,支气管扩张作用和毛发生长刺激作用。
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